IP Library Granted Patent US 7,138,411
Granted Patent B2
US 7,138,411 · App. 10/303,150 · Granted Nov 21, 2006

Substituted benzopyran derivatives for the treatment of inflammation

Assignee: G.D. Searle & Co.
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Quick Facts
Patent No.
US 7,138,411
App. No.
10/303,150
Granted
Nov 21, 2006
Kind
B2
Abstract

A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A 1 , A 2 , A 3 , A 4 , R, R″, R 1 and R 2 are as described in the specification.

Claims (17)

1. A compound of Formula I

wherein X is selected from O, S, or NR a ;

wherein R is selected from carboxyl, aminocarbonyl, C 1 –C 6 -alkylsulfonylaminocarbonyl and C 1 –C 6 -alkoxycarbonyl;

wherein R 1 is selected from alkyl, aralkyl, cycloalkyl or aryl optionally substituted with one or more radicals selected from alkylthio, nitro and alkylsulfonyl;

wherein R 2 is one or more radicals independently selected from hydrido, halo, aralkyl, alkoxy, aryloxy, heteroaryloxy, aralkyloxy, heteroaralkyloxy, haloalkyl, haloalkoxy, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroarylalkylamino, nitro, amino, aminosulfonyl, alkylaminosulfonyl, arylaminosulfonyl, heteroarylaminosulfonyl, aralkylaminosulfonyl, heteroaralkylaminosulfonyl, heterocyclosulfonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heteroaryl, aralkylcarbonyl, heteroarylcarbonyl, arylcarbonyl, aminocarbonyl and alkylcarbonyl; and

or wherein R 2 together with ring A forms radical;

or an isomer or pharmaceutically acceptable salt thereof.

2. A compound of Formula

wherein R 1 is selected from alkyl, aralkyl, cycloalkyl or aryl optionally substituted with one or more radicals selected from alkylthio, nitro and alkylsulfonyl; and

wherein R 2 is one or more radicals independently selected from hydrido, halo, aralkyl, alkoxy, aryloxy, heteroaryloxy, aralkyloxy, heteroaralkyloxy, haloalkyl, haloalkoxy, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroarylalkylamino, nitro, amino, aminosulfonyl, alkylaminosulfonyl, arylaminosulfonyl, heteroarylaminosulfonyl, aralkylaminosulfonyl, heteroaralkylaminosulfonyl, heterocyclosulfonyl, alkylsulfonyl, optionally substituted aryl, optionally substituted heteroaryl, aralkylcarbonyl, heteroarylcarbonyl, arylcarbonyl, aminocarbonyl and alkylcarbonyl;

or an isomer or pharmaceutically acceptable salt thereof.

3. A method of treating a cyclooxygenase-2 mediated disorder in a subject, said method comprising treating the subject having or susceptible to said disorder with a therapeutically-effective amount of a compound of claim 1 ; or a pharmaceutically-acceptable salt thereof.

4. The method of claim 3 wherein the cyclooxygenase-2 mediated disorder is inflammation.

5. The method of claim 3 wherein the cyclooxygenase-2 mediated disorder is arthritis.

6. The method of claim 3 wherein the cyclooxygenase-2 mediated disorder is pain.

7. The method of claim 3 wherein the cyclooxygenase-2 mediated disorder is cancer.

8. A pharmaceutical composition comprising a therapeutically-effective amount of a compound of claim 1 , or a pharmaceutically-acceptable salt thereof, and a pharmaceutically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2012
From: G.D. SEARLE, LLC
To: RAQUALIA PHARMA INC.
Reel/Frame 027961/0801 →
CHANGE OF NAME Recorded Jan 27, 2012
From: G.D. SEARLE & CO.
To: G.D. SEARLE LLC
Reel/Frame 027609/0264 →
Continuity (6)
Continuation 0986517700 · May 24, 2001
Continuation 0956938300 · May 11, 2000
Continuation 0917558400 · Oct 20, 1998
Continuation In Part 0906253700 · Apr 17, 1998
Provisional Application 6004448500 · Apr 21, 1997
Related Publication 20040038977A1 · Feb 26, 2004